Technical Field
This invention is directed to a novel variable hydrate crystalline form of Compound (I) as described herein, methods for the preparation thereof, pharmaceutical compositions thereof, and their use as a PDE10 inhibitor.
Description of the Related Art
Compound (I), 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, is a PDE10 inhibitor.
Compound (I) falls within the scope of PDE10 inhibitors disclosed in International PCT Application Publication No. WO 2011/112828. Compound (I) is specifically disclosed as compound no. 65-10 in International PCT Application No. WO 2011/112828. Compound (I) can be prepared according to the general procedures found in International PCT Application Publication No. WO 2011/112828, which are herein incorporated by reference.
In drug development, it is necessary to produce a compound that can enable a formulation to meet targeted pharmaceutical requirements and specifications. This may be achieved through the use of a stable crystalline form (sometimes referred to as a polymorph) of the drug. It is desirable to select a drug form that is easily and consistently manufactured, has good handling characteristics suitable for large-scale manufacturing and in formulating dosage forms so that it can be produced on a large-scale in a cost-efficient manner, is sufficiently shelf-stable such that does not change polymorphic form during manufacturing, shipment, or storage, and has suitable bioavailability and release characteristics. The present invention fulfills these needs and provides further related advantages.